Idebenone is a synthetic short-chain benzoquinone and a substrate for the enzyme NAD(P)H:quinone oxidoreductase (NQO1) capable of stimulating mitochondrial electron transport and supplementing cellular energy levels. Idebenone was initially developed by Takeda Pharmaceutical Company for the treatment of Alzheimer’s disease and other cognitive defects. This has been met with limited success. The Swiss company Santhera Pharmaceuticals has started to investigate it for the treatment of neuromuscular diseases. In 2010, early clinical trials for the treatment of Friedreich’s ataxia and Duchenne muscular dystrophy have been completed. In clinical trials, Idebenone (Raxone/Catena) had a positive impact on a measurement of respiratory function (Peak Expiratory Flow, or PEF) in non-ambulatory Duchenne muscular dystrophy patients who were not taking steroids. As of December 2013 the drug is not approved for these indications in North America or Europe. It is approved for the treatment of Leber's hereditary optic neuropathy (LHON) in Europe. Idebenone (Raxone) is indicated for the treatment of visual impairment in adolescent and adult patients with Leber’s Hereditary Optic Neuropathy (LHON). Because the number of patients with Leber's hereditary optic neuropathy is low, the disease is considered ‘rare’, and Raxone was designated an ‘orphan medicine’ on 15 February 2007. Idebenone is thought to help improve production of energy by restoring mitochondrial function, thereby preventing the cellular damage and the loss of sight seen in LHON. Idebenone is a rapidly absorbed, safe and well-tolerated drug and is currently the only clinically proven treatment option for Leber's hereditary optic neuropathy (LHON) patients.

2,5-Dimethyl-N-Phenyl-3H-diazaphophol-4-imine is a quinonoid tautomer of GABAA and GABAB agonist progabide. According to quantum mechanical calculations, a quinonoid form is predominant in polar solvents, while aromatic tautomer is prevalent in apolar solvents. Progabide is a prodrug of gamma-aminobutyric acid and was investigated for the treatment of epilepsy, Parkinson's disease, schizophrenia, clinical depression, anxiety disorder, and other diseases. Progabide was marketed in France by Sanofi Aventis under tradename Gabrene for use in monotherapy and also as adjunctive therapy for generalized tonic-clonic, myoclonic, partial seizures, and for Lennox‐Gastaut syndrome, in both children and adults.

Bifemelane is a psychotropic drug, was found to inhibit monoamine oxidase (MAO). It inhibited type A MAO (MAO-A) competitively and type B (MAO-B) noncompetitively and it was a more potent inhibitor of MAO-A than of MAO-B. Bifemelane is an antidepressant and cerebral activator that is used in Japan for the treatment of cerebral infarction patients with depressive symptoms, and in the treatment of senile dementia as well. It also appears to be useful in the treatment of glaucoma.

Lofepramine is a tricyclic antidepressant that is structurally similar to imipramine and is extensively metabolised to desipramine. In the absence of other major pharmacological effects it appears that its antidepressant activity stems from the facilitation of noradrenergic neurotransmission by uptake inhibition, and possibly by the additional facilitation of serotoninergic neurotransmission. The overall therapeutic efficacy of lofepramine is comparable to that of imipramine, amitriptyline, clomipramine, maprotiline and mianserin in patients with depression of varying severity, and coexisting anxiety. Lofepramine is a strong inhibitor of norepinephrine reuptake (Ki=5.4 nM) and a moderate inhibitor of serotonin reuptake (Ki=70 nM). It is a weak-intermediate level antagonist of the muscarinic acetylcholine receptors.Lofepramine is licensed for the treatment of depression in the United Kingdom.

Iprazochrome is a serotonin antagonist both in vitro and in vivo. It is used in the prophylaxis of migraine and in the treatment of diabetic retinopathy.

Iproclozide [1-(p-chlorophenoxyacetyl)-2-isopropylhydrazine] is a non-selective monoamine oxidase inhibitor. It has been used in the treatment of depressive states. Iproclozide was studied in the treatment of hypertension and angina pectoris. It may induce fatal hepatitis.

Fabomotizole (also known as Afobazole) is a selective non-benzodiazepine anxiolytic which was developed in Russia and launched in 2006. The drug is used for the treatment of wide range of diseases: generalized anxious disorders, neurasthenia, adaptation disorders, sleep disorders, for alleviation of withdrawal syndrome. According to the drug label (in Russian), its action is related to the interaction with sigma-1 receptors.

Cinolazepam is a drug which is a benzodiazepine derivative. It possesses anxiolytic, anticonvulsant, sedative and skeletal muscle relaxant properties. Cinolazepam is not approved for sale in the United States or Canada. Cinolazepam binds to central benzodiazepine receptors, which interact allosterically with GABA receptors. This potentiates the effects of the inhibitory neurotransmitter GABA, increasing the inhibition of the ascending reticular activating system and blocking the cortical and limbic arousal that occurs following stimulation of the reticular pathways. Statistical analyses of objective sleep variables in men demonstrated a significant improvement of sleep maintenance after cinolazepam as reflected by an increase of sleep efficiency, decrease of wake time (during total sleep period) and number of awakenings as compared with the placebo. It is indicated for the treatment of sleep disorders of different etiologies.

Adinazolam, a benzodiazepine agonist, is an effective anxiolytic agent with antidepressant properties. It was shown, that adinazolam by itself had relatively weak benzodiazepine agonist activity, and much of the pharmacological activity belonged to its active metabolite N-desmethyladinazolam (NDMAD). Adinazolam has never been FDA approved, but it is sold as a research chemical.

Scientists at Parke-Davis first synthesized Pramiracetam (brand name Pramistar) in the late 1970’s. It was first tested with Alzheimer’s patients. Seeing mixed results, the company tried it with major depressive disorder and licensed it as an orphan drug to Menarini. Pramiracetam is a central nervous system stimulant and nootropic agent belonging to the racetam family of drugs. Pramistar is used for the treatment of concentration and memory disturbances caused by the degeneration of brain cells or to diseases of the blood vessels supplying the brain, conditions that arise both in elderly patients (aged over 65 years). By stimulating choline uptake, pramiracetam indirectly modulates the release of acetylcholine and stimulates increased activity in the hippocampus. Because this part of the brain is absolutely crucial to the memory function, the general stimulation that pramiracetam creates can improve both the formation of new memories and the retention of reference or long-term memories. The increased activity in the hippocampus also increases cerebral blood flow, which enhances alertness and improves cognitive abilities in general. Pramiracetam may have other mechanisms of action as well. Researchers have hypothesized that in addition to its action in the brain, pramiracetam acts outside the brain in peripheral sites that rely on the adrenal glands. Animal studies suggest that pramiracetam may also increase or restore brain membrane fluidity, which facilitates cell signaling. Unlike many other racetam class nootropics, pramiracetam does not appear to strongly alter either wakefulness or emotional states. This can be explained by pramiracetam’s very limited influence on the production and release of serotonin, GABA and dopamine, the neurotransmitters that have the greatest effect on mood and anxiety levels.